PI3Kα/CDK7-IN-1
PI3Kα/CDK7-IN-1 is a dual-target hybrid inhibitor of PI3Kα and CDK7, with IC50 values of 87.9 nM and 638 nM, respectively. PI3Kα/CDK7-IN-1 acts as a cytotoxic agent and cell death inducer that triggers apoptotic death in cancer cells. PI3Kα/CDK7-IN-1 can be used in cancer research such as colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C26H25F3N9O3PS
- Molecular Weight:631.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PI3Kα 87.9 nM (IC50) |
CDK7 638 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
360 nM
|
Cytotoxicity against human HCT116 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
Cytotoxicity against human HCT116 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
|
42468711 |
| SK-OV-3 | IC50 |
490 nM
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Cytotoxicity against human SKOV3 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
Cytotoxicity against human SKOV3 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
|
42468711 |
| MCF7 | IC50 |
820 nM
|
Cytotoxicity against human MCF7 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
Cytotoxicity against human MCF7 cancer cells (carrying activating PI3Kα driver mutation) assessed as reduction in cell viability via 10-point titration for IC50 determination.
|
42468711 |
PI3Kα/CDK7-IN-1 (Compound HY5) inhibits the viability of HCT116, SKOV3 and MCF7 cancer cells carrying PI3Kα mutations, with IC50 values of 360 nM, 490 nM and 820 nM, respectively[1].
PI3Kα/CDK7-IN-1 reduces the viability of MDA-MB-231, U2OS and NCI-H522 cancer cells, and exhibits stronger activity against NCI-H522 cells overexpressing SLC7A11[1].
PI3Kα/CDK7-IN-1 (10 μM; 48 h) alters cell cycle progression, induces apoptosis and non-apoptotic cell death, and triggers cellular stress responses in HCT116 cells, as evidenced by increased phosphorylation levels of CDK/MAPK substrates, reduced mitotic index, upregulated levels of activated caspase-3, and formation of pyknotic nuclei[1].
PI3Kα/CDK7-IN-1 (10 μM; 48 h) induces cellular stress responses in HCT116 cells[1].
PI3Kα/CDK7-IN-1 (5-10 μM; 24-48 h) reduces the viability of HCT116 cells through both caspase-dependent apoptotic and non-apoptotic mechanisms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colon cancer cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Increased global phosphorylation of CDK and MAPK substrates.
Caused a ~2-fold increase in DAPI staining intensity.
Reduced the mitotic index to undetectable levels.
Induced a slight but significant decrease in RB phosphorylation at serine 780.
Increased cleaved caspase-3-positive cells to 17% compared to vehicle-treated cells.
Chemical Information
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Molecular Weight 631.57
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Formula C26H25F3N9O3PS
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SMILES
FC(F)(C(C=NC(NC1=C(N=C(NC(N(CCC2)C2C(N)=O)=O)S1)C)=N3)=C3C4=CNC5=C4C=CC(C#N)=C5P(C)(C)=O)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)